DK3351539T3 - Crystalline monohydrate complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(beta-d-glucopyranos-1-yl)-benzene and proline in crystal water (1:1:1), methods for its preparation and its use as an SGLT inhibitor - Google Patents

Crystalline monohydrate complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(beta-d-glucopyranos-1-yl)-benzene and proline in crystal water (1:1:1), methods for its preparation and its use as an SGLT inhibitor Download PDF

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Publication number
DK3351539T3
DK3351539T3 DK18155079.9T DK18155079T DK3351539T3 DK 3351539 T3 DK3351539 T3 DK 3351539T3 DK 18155079 T DK18155079 T DK 18155079T DK 3351539 T3 DK3351539 T3 DK 3351539T3
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glucopyranos
proline
cyclopropyl
cyano
beta
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DK18155079.9T
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Danish (da)
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Matthias Eckhardt
Tanja Maria Butz
Frank Himmelsbach
Hans-Juergen Martin
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Boehringer Ingelheim Vetmedica Gmbh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26Acyclic or carbocyclic radicals, substituted by hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/10Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04Carbocyclic radicals

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
DK18155079.9T 2012-07-26 2013-07-25 Crystalline monohydrate complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(beta-d-glucopyranos-1-yl)-benzene and proline in crystal water (1:1:1), methods for its preparation and its use as an SGLT inhibitor DK3351539T3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12177944 2012-07-26
EP13740309.3A EP2877460B1 (en) 2012-07-26 2013-07-25 CRYSTALLINE COMPLEX OF 1-CYANO-2-(4-CYCLOPROPYL-BENZYL)-4-(ß-D-GLUCOPYRANOS-1-YL)-BENZENE, METHODS FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS

Publications (1)

Publication Number Publication Date
DK3351539T3 true DK3351539T3 (en) 2023-01-30

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Family Applications (2)

Application Number Title Priority Date Filing Date
DK18155079.9T DK3351539T3 (en) 2012-07-26 2013-07-25 Crystalline monohydrate complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(beta-d-glucopyranos-1-yl)-benzene and proline in crystal water (1:1:1), methods for its preparation and its use as an SGLT inhibitor
DK13740309.3T DK2877460T3 (en) 2012-07-26 2013-07-25 CRYSTALLINE COMPLEX OF 1-CYANO-2-(4-CYCLOPROPYL-BENZYL)-4-(ß-D-GLUCOPYRANOS-1-YL)-BENZENE, METHODS FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS.

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DK13740309.3T DK2877460T3 (en) 2012-07-26 2013-07-25 CRYSTALLINE COMPLEX OF 1-CYANO-2-(4-CYCLOPROPYL-BENZYL)-4-(ß-D-GLUCOPYRANOS-1-YL)-BENZENE, METHODS FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS.

Country Status (23)

Country Link
US (1) US9145434B2 (en)
EP (3) EP2877460B1 (en)
JP (2) JP6538556B2 (en)
CN (2) CN108774200A (en)
AR (1) AR091908A1 (en)
AU (1) AU2013294947B2 (en)
BR (1) BR112015001327B1 (en)
CA (1) CA2878698C (en)
DK (2) DK3351539T3 (en)
EA (2) EA025438B1 (en)
ES (2) ES2937665T3 (en)
FI (1) FI3351539T3 (en)
HR (2) HRP20230081T1 (en)
HU (1) HUE061450T2 (en)
LT (1) LT3351539T (en)
MX (1) MX357906B (en)
PL (2) PL2877460T3 (en)
PT (2) PT3351539T (en)
RS (1) RS63881B1 (en)
SG (1) SG11201500574QA (en)
SI (2) SI2877460T1 (en)
TW (1) TW201418275A (en)
WO (1) WO2014016381A1 (en)

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EP4245765A3 (en) 2013-04-04 2024-03-20 Boehringer Ingelheim Vetmedica GmbH Treatment of metabolic disorders in equine animals
DK3082829T3 (en) 2013-12-17 2021-05-03 Boehringer Ingelheim Vetmedica Gmbh SGLT2 INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS IN CATS
DK3096765T3 (en) 2014-01-23 2019-03-04 Boehringer Ingelheim Vetmedica Gmbh Treatment of metabolic disorders in dogs
ES2811261T3 (en) * 2014-04-01 2021-03-11 Boehringer Ingelheim Vetmedica Gmbh Treatment of metabolic disorders in equine animals
CN103965020B (en) * 2014-05-06 2015-09-09 启东东岳药业有限公司 Prepare the method for 5-iodo-2-bromobenzyl alcohol
WO2016046150A1 (en) * 2014-09-25 2016-03-31 Boehringer Ingelheim Vetmedica Gmbh Combination treatment of sglt2 inhibitors and dopamine agonists for preventing metabolic disorders in equine animals
BR112017005454A2 (en) * 2014-09-30 2017-12-12 Jiangsu Hengrui Medicine Co sodium glucose transporter inhibitor 2 l-proline compound, and l-proline compound monohydrate and crystal
CZ2015110A3 (en) * 2015-02-18 2016-08-31 Zentiva, K.S. Empagliflozin solid forms
AU2016310535B2 (en) 2015-08-27 2021-08-19 Boehringer Ingelheim Vetmedica Gmbh Liquid pharmaceutical compositions comprising SGLT-2 inhibitors
WO2017203457A1 (en) * 2016-05-26 2017-11-30 Dr. Reddy's Laboratories Limited Solid state forms of empagliflozin
JP6785523B2 (en) * 2016-05-28 2020-11-18 ジ・リン・フイ・シェン・バイオ−ファーマシューティカル・カンパニー・リミテッドJi Lin Hui Sheng Bio−Pharmaceutical Co., Ltd. Crystal form of sodium-glucose cotransporter 2 inhibitor
EA202091466A1 (en) 2017-12-19 2020-10-23 Бёрингер Ингельхайм Ветмедика Гмбх SYNTHESIS OF SOCRYSTAL 1: 1: 1 1-CIANO-2- (4-CYCLOPROPYLBENZYL) -4 - (- D-GLUCOPYRANOSE-1-YL) BENZENE, L-PROLINE AND WATER
BR112022010385A2 (en) 2019-11-28 2022-08-23 Boehringer Ingelheim Vetmedica Gmbh USE OF SGLT-2 INHIBITORS IN THE DRYING OF NON-HUMAN MAMMALS
EP4106744A1 (en) 2020-02-17 2022-12-28 Boehringer Ingelheim Vetmedica GmbH Use of sglt-2 inhibitors for the prevention and/or treatment of cardiac diseases in felines
KR20240041966A (en) 2021-07-28 2024-04-01 베링거잉겔하임베트메디카게엠베하 Use of SGLT-2 inhibitors for the prevention and/or treatment of cardiac disease in non-human mammals other than cats, especially dogs
CN117715639A (en) 2021-07-28 2024-03-15 勃林格殷格翰动物保健有限公司 Use of SGLT-2 inhibitors for the prevention and/or treatment of kidney disease in non-human mammals
EP4376819A1 (en) 2021-07-28 2024-06-05 Boehringer Ingelheim Vetmedica GmbH Use of sglt-2 inhibitors for the prevention and/or treatment of hypertension in non-human mammals
WO2023227492A1 (en) 2022-05-25 2023-11-30 Boehringer Ingelheim Vetmedica Gmbh Aqueous pharmaceutical compositions comprising sglt-2 inhibitors

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EP1385856B1 (en) * 2001-04-11 2006-02-22 Bristol-Myers Squibb Company Amino acid complexes of c-aryl glucosides for treatment of diabetes and method
US7927613B2 (en) * 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
EP1581543A4 (en) * 2003-01-03 2008-03-19 Bristol Myers Squibb Co Methods of producing c-aryl glucoside sglt2 inhibitors
SG151271A1 (en) * 2004-03-16 2009-04-30 Boehringer Ingelheim Int Glucopyranosyl-substituted benzol derivatives, drugs containing said compounds, the use thereof and method for the production thereof
JP5345846B2 (en) * 2005-09-08 2013-11-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Crystal form of 1-chloro-4- (β-D-glucopyranos-1-yl) -2- (4-ethynyl-benzyl) -benzene, process for its preparation and their use for the manufacture of a medicament
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EP4245765A3 (en) 2013-04-04 2024-03-20 Boehringer Ingelheim Vetmedica GmbH Treatment of metabolic disorders in equine animals

Also Published As

Publication number Publication date
PL2877460T3 (en) 2019-04-30
ES2694675T3 (en) 2018-12-26
HRP20230081T1 (en) 2023-03-17
HUE061450T2 (en) 2023-07-28
BR112015001327A2 (en) 2017-07-04
CN104470908A (en) 2015-03-25
SI3351539T1 (en) 2023-03-31
PL3351539T3 (en) 2023-03-06
SI2877460T1 (en) 2018-12-31
PT3351539T (en) 2023-01-17
AU2013294947A1 (en) 2015-01-22
MX357906B (en) 2018-07-30
ES2937665T3 (en) 2023-03-30
BR112015001327B1 (en) 2022-08-16
FI3351539T3 (en) 2023-02-19
EP3351539A1 (en) 2018-07-25
CN108774200A (en) 2018-11-09
RS63881B1 (en) 2023-02-28
SG11201500574QA (en) 2015-02-27
JP2018135384A (en) 2018-08-30
AU2013294947B2 (en) 2017-03-30
DK2877460T3 (en) 2019-01-07
HRP20181972T1 (en) 2019-01-25
JP2015522644A (en) 2015-08-06
PT2877460T (en) 2018-12-19
MX2015000962A (en) 2015-04-16
WO2014016381A1 (en) 2014-01-30
TW201418275A (en) 2014-05-16
AR091908A1 (en) 2015-03-11
EP2877460B1 (en) 2018-09-12
LT3351539T (en) 2023-02-10
EP4166548A1 (en) 2023-04-19
US9145434B2 (en) 2015-09-29
CA2878698C (en) 2021-03-23
US20140031540A1 (en) 2014-01-30
CA2878698A1 (en) 2014-01-30
EA201600506A1 (en) 2017-03-31
JP6538556B2 (en) 2019-07-03
EA201500038A1 (en) 2015-07-30
EP3351539B1 (en) 2022-11-09
EA025438B1 (en) 2016-12-30
EP2877460A1 (en) 2015-06-03

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